Preparation of sustained release pharmaceutical composition

Abstract

A sustained release apparatus including a silicone support material; and a pharmaceutically active composition carried in or on the silicone support material; the pharmaceutically active composition including at least one pharmaceutically active component; and optionally a carrier therefor; the pharmaceutically active component being present in amounts of from approximately 30% to 75% by weight, based on the total weight of the sustained release apparatus.

1 - 77 . Cancelled.  
     
     
         78 . A sustained release apparatus including 
 a silicone support material; and    a pharmaceutically active composition carried in or on the silicone support material;    the pharmaceutically active composition including 
 at least one pharmaceutically active component; and optionally  
 a carrier therefor;  
   the pharmaceutically active component being present in amounts of from approximately 30% to 75% by weight, based on the total weight of the sustained release apparatus.    
     
     
         79 . A sustained release apparatus according to  claim 78 , wherein the apparatus is of the uncovered or covered rod, or dispersed matrix type.  
     
     
         80 . A sustained release apparatus according to  claim 79 , wherein the apparatus takes the form of a rod bearing a silicone coating thereover.  
     
     
         81 . A sustained release apparatus according to  claim 78 , wherein the pharmaceutically active component is present in amounts of from approximately 40% to 50% by weight, based on the total weight of the apparatus.  
     
     
         82 . A sustained release apparatus according to  claim 78 , wherein the silicone support material is formed from a silicone base polymer.  
     
     
         83 . A sustained release apparatus according to  claim 82 , wherein the silicone base polymer includes a methyl-vinyl polysiloxane polymer.  
     
     
         84 . A sustained release apparatus according to  claim 82 , wherein the silicone base polymer includes a silicone elastomer including a fumed silica as reinforcing filler.  
     
     
         85 . A sustained release apparatus according to  claim 82 , wherein the silicone base polymer is present in amounts of from approximately 15% to 70% by weight, based on the total weight of the apparatus.  
     
     
         86 . A sustained release apparatus according to  claim 78 , wherein the pharmaceutically active composition includes a pharmaceutically active component selected from one or more of the group consisting of acetonemia preparations, anabolic agents, anaesthetics, analgesics, anti-acid agents, anti-arthritic agents, antibodies, anti-convulsivants, anti-fungals, anti-histamines, anti-infectives, anti-inflammatories, anti-microbials, anti-parasitic agents, anti-protozoals, anti-ulcer agents, antiviral pharmaceuticals, behaviour modification drugs, biologicals, blood and blood substitutes, bronchodilators and expectorants, cancer therapy and related pharmaceuticals, cardiovascular pharmaceuticals, central nervous system pharmaceuticals, coccidiostats and coccidiocidals, contraceptives, contrast agents, diabetes therapies, diuretics, fertility pharmaceuticals, growth hormones, growth promoters, hematinics, hemostatics, hormone replacement therapies, hormones and analogs, immunostimulants, minerals, muscle relaxants, natural products, nutraceuticals and nutritionals, obesity therapeutics, ophthalmic pharmaceuticals, osteoporosis drugs, pain therapeutics, peptides and polypeptides, respiratory pharmaceuticals, sedatives and tranquilizers, transplantation products, urinary acidifiers, vaccines and adjuvants and vitamins.  
     
     
         87 . A sustained release apparatus according to  claim 86 , wherein the pharmaceutically active component includes an anti-parasitic agent which includes ivermectin.  
     
     
         88 . A sustained release apparatus including 
 a silicone support material; and    an anthelmintic composition carried in or on the support material;    the anthelmintic composition including 
 an anthelmintic component; and optionally  
 a carrier therefor;  
   the anthelmintic component being present in amounts of from approximately 30% to 75% by weight, based on the total weight of the apparatus.    
     
     
         89 . A sustained release apparatus according to  claim 88 , wherein the anthelmintic component includes ivermectin.  
     
     
         90 . A process for the preparation of a sustained release apparatus including 
 a silicone support material; and    a pharmaceutically active composition carried in or on the silicone support material;    the pharmaceutically active composition including 
 at least one pharmaceutically active component; and optionally  
 a carrier therefor;  
   the pharmaceutically active component being present in amounts of from approximately 30% to 75% by weight, based on the total weight of the sustained release apparatus, which process includes    providing 
 a silicone base polymer;  
 a cross-linking agent;  
 a pharmaceutically active component;  
 a peroxide or metal catalyst; and  
 a low temperature curing inhibitor;  
   pre-mixing at least a portion of the silicone base polymer and the metal catalyst together to form a first part;    pre-mixing the cross-linking agent, low temperature curing inhibitor, any remaining silicone base polymer, and pharmaceutical active for a time sufficient to at least partially wet the pharmaceutical active and form a second part; and    mixing the first and second parts together as a batch or continuously; and    feeding the mixture into a molding or extrusion apparatus at a relatively low temperature for a relatively short time sufficient to permit the components to cure to form the sustained release apparatus.    
     
     
         91 . A process according to  claim 90 , wherein the silicone base polymer includes a methyl-vinyl siloxane polymer.  
     
     
         92 . A process according to  claim 90 , wherein the silicone base polymer further includes a reinforcing filler.  
     
     
         93 . A process according to  claim 90 , wherein the cross-linking agent includes a partially hydrogenated polysiloxane polymer.  
     
     
         94 . A process according to  claim 90 , wherein the catalyst is a platinum catalyst present in amounts of from approximately 0.05% to 0.25%, by weight, based on the total weight of the reaction mixture.  
     
     
         95 . A process according to  claim 90 , wherein the low temperature curing inhibitor includes a tetramethyl tetra-vinyl cyclosiloxane.  
     
     
         96 . A process according to  claim 90 , further including 
 providing a carrier for the pharmaceutically active component in an amount of from approximately 15% to 25% by weight based on the total weight of the reaction mixture; and    pre-mixing the pharmaceutical carrier in the first part.    
     
     
         97 . A process according to  claim 96 , wherein the pharmaceutical carrier includes sodium chloride or mannitol or mixtures thereof.  
     
     
         98 . A process according to  claim 90 , wherein a portion of the pharmaceutically active component is included in the first part.  
     
     
         99 . A process according to  claim 90 , further including 
 providing 
 a liquid coating composition including 
 a liquid silicone base material;  
 a cross-linking agent; and  
 metal catalyst  
 
   coating the apparatus with the coating composition; and    heating the coated apparatus to a temperature and for a time sufficient to cure the coating layer.    
     
     
         100 . A biocompatible article including a sustained release apparatus including 
 a silicone support material; and    a pharmaceutically active composition carried in or on the silicone support material;    the pharmaceutically active composition including 
 at least one pharmaceutically active component; and optionally  
 a carrier therefor;  
   the pharmaceutically active component being present in amounts of from approximately 30% to 75% by weight, based on the total weight of the sustained release apparatus.    
     
     
         101 . A biocompatible article according to  claim 100 , wherein the pharmaceutically active component is present in amounts from approximately 40% to 50% by weight, based on the total weight of the sustained release apparatus.  
     
     
         102 . A biocompatible article according to  claim 100 , wherein the biocompatible article is a medical instrument, apparatus or prosthetic device or part thereof.  
     
     
         103 . A biocompatible article according to  claim 102 , wherein the biocompatible article is a catheter, prosthetic appliance or medical implant for reconstructive dental or cosmetic surgery.  
     
     
         104 . A biocompatible article according to  claim 100 , wherein the pharmaceutically active component includes an anti-coagulation agent an anti-anginal agent.  
     
     
         105 . A method for the therapeutic or prophylactic treatment of a disease condition in an animal (including a human) requiring such treatment, which method includes administering to the animal a sustained release apparatus including 
 a silicone support material; and    a pharmaceutically active composition carried in or on the silicone support material;    the pharmaceutically active composition including 
 at least one pharmaceutically active component; and optionally  
 a carrier therefor;  
   the pharmaceutically active component being present in amounts ranging from 30 to 75% by weight, based on the total weight of the sustained release apparatus.    
     
     
         106 . A method according to  claim 105 , wherein the pharmaceutically active component is present in amounts ranging from 40% to 50% by weight, based on the total weight of the apparatus.  
     
     
         107 . A method according to  claim 105 , wherein the sustained release apparatus forms part of a biocompatible article.